SML0486

依克立达

Name: 依克立达
Brand: SIGMA

≥98% (HPLC), powder, ABC transporters MDR-1 (P-gp) inhibitor

同義詞:

GF120918, GG918, GW0918, N-[4-[2-（3,4-二氢-6,7-二甲氧基-2 (1H)-异喹啉基）乙基] 苯基]-9,10-二氢-5-甲氧基-9-氧代-4-吖啶甲酰胺

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關於此項目

經驗公式（希爾表示法）:

C₃₄H₃₃N₃O₅

CAS 編號:

143664-11-3

分子量：:

563.64

UNSPSC Code:

12161501

PubChem Substance ID:

329825437

NACRES:

NA.77

MDL number:

MFCD00912604

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產品名稱

依克立达, ≥98% (HPLC)

SMILES string

COc1cccc2C(=O)c3cccc(C(=O)Nc4ccc(CCN5CCc6cc(OC)c(OC)cc6C5)cc4)c3Nc12

InChI

1S/C34H33N3O5/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38)

InChI key

OSFCMRGOZNQUSW-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL (clear solution, warmed)

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

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Show Differences

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本產品	SML1297	SML1790	SML1184
Sigma-Aldrich SML0486 依克立达	Sigma-Aldrich SML1297 SB269652	Sigma-Aldrich SML1790 他立喹达	Sigma-Aldrich SML1184 OF-1
form powder	form powder	form powder	form powder
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. −20°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 2 mg/mL (clear solution, warmed)	solubility DMSO: 2 mg/mL	solubility DMSO: 10 mg/mL, clear	solubility DMSO: 5 mg/mL, clear (warmed)
shipped in wet ice	shipped in -	shipped in -	shipped in -

Application

依克立达（Elacridar）可用作：

作为化学物质，解释自噬作用与舒尼替尼耐药机制之间的联系[1]
作为 ATP 结合盒 B亚家族1成员的抑制剂，研究其对 NSC23766细胞毒性的作用[2]
处理罗丹明123（Rh123）标记细胞，在荧光激活细胞分选法（FACS）中设置分选门 [3]

Biochem/physiol Actions

GF120918（依克立达）是 ABC 转运蛋白 MDR-1 (P-gp) 和 BCRP 的强效抑制剂。GF120918 可增加细胞毒性抗肿瘤药物的生物利用度，也可导致大脑和 CNS 中抗 HIV 药物水平升高。

GF120918（依克立达）是一种 MDR-1 (P-gp) 抑制剂。

Features and Benefits

这种化合物是 ADME 毒性研究的特色产品。点击此处发现更多特色 ADME 毒性产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

存儲類別/等級

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

從最近期的版本中選擇一個：

分析證明 (COA)

Lot/Batch Number

0000516659

0000464197

0000424769

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Saturable active efflux by p-glycoprotein and breast cancer resistance protein at the blood-brain barrier leads to nonlinear distribution of elacridar to the central nervous system.

Ramola Sane et al.

The Journal of pharmacology and experimental therapeutics, 345(1), 111-124 (2013-02-12)

The study objective was to investigate factors that affect the central nervous system (CNS) distribution of elacridar. Elacridar inhibits transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) and has been used to study the influence of transporters

The influence of modulation of P-glycoprotein and /or cytochrome P450 3A on the pharmacokinetics and pharmacodynamics of orally administered morphine in dogs.

C Gadeyne et al.

Journal of veterinary pharmacology and therapeutics, 34(5), 417-423 (2011-01-19)

The influence of pretreatment with ketoconazole [cytochrome P450 3A (CYP3A) + P-glycoprotein (P-gp) inhibitor], elacridar (selective P-gp inhibitor) and rifampicin (CYP3A + P-gp inducer) on oral morphine pharmacokinetics and pharmacodynamics was investigated in experimental dogs. Seven beagles were used in

Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar.

Selvi Durmus et al.

Molecular pharmaceutics, 9(11), 3236-3245 (2012-10-02)

Vemurafenib (PLX4032) is a novel tyrosine kinase inhibitor that has clinical efficacy against metastatic melanoma harboring a BRAF(V600E) mutation. We aimed to establish whether oral availability and brain penetration of vemurafenib could be restricted by the multidrug efflux transporters P-glycoprotein

Dual approach utilizing self microemulsifying technique and novel P-gp inhibitor for effective delivery of taxanes.

Akash Chaurasiya et al.

Journal of microencapsulation, 29(6), 583-595 (2012-03-24)

In the present work, concomitant use of self-microemulsifying drug delivery systems (SMEDDS) and a novel third-generation P-gp inhibitor, GF120918 (elacridar), for the effective transport of taxanes (paclitaxel and docetaxel) across an in vitro model of the intestinal epithelium and uptake into

Hepatic basolateral efflux contributes significantly to rosuvastatin disposition I: characterization of basolateral versus biliary clearance using a novel protocol in sandwich-cultured hepatocytes.

Nathan D Pfeifer et al.

The Journal of pharmacology and experimental therapeutics, 347(3), 727-736 (2013-09-12)

Transporters responsible for hepatic uptake and biliary clearance (CLBile) of rosuvastatin (RSV) have been well characterized. However, the contribution of basolateral efflux clearance (CLBL) to hepatic and systemic exposure of RSV is unknown. Additionally, the appropriate design of in vitro

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